Folate-targeted nanoparticle delivery of androgen receptor shRNA enhances the sensitivity of hormone-independent prostate cancer to radiotherapy

Nanomedicine. 2017 May;13(4):1309-1321. doi: 10.1016/j.nano.2017.01.015. Epub 2017 Feb 6.

Abstract

Androgen receptor (AR) plays a crucial role in the development and progression of prostate cancer (PCa). PCa patients typically receive androgen deprivation therapy; nonetheless, these patients eventually develop castration and radiation resistance. We hypothesized that we could further improve radiotherapeutic efficacy of hormone-independent PCa (HIPC) by silencing AR. In this study, nanoparticle (NP) AR-shRNA was formulated using folate-targeted H1 nanopolymer. We demonstrated that NP AR-shRNA enhances PCa radiosensitivity as indicated by the inhibition of cell growth, increased apoptosis, and increased cell cycle arrest in AR-dependent HIPC in vitro. The radiosensitizing effect of NP AR-shRNA could be validated in vivo, as NP AR-shRNA significantly suppressed tumor growth and prolonged the survival of HIPC tumor-bearing mice. Analysis at the molecular level revealed that NP AR-shRNA inhibits DNA damage repair signaling pathways. Our study supports further investigation of NP AR-shRNA for the improvement of radiotherapy efficacy in HIPC.

Keywords: Androgen receptor interference; Hormone-independent prostate cancer; Nanoparticle; Radiosensitivity; Subcutaneous xenotransplanted tumor model.

MeSH terms

  • Androgen Receptor Antagonists / therapeutic use*
  • Animals
  • Cell Line, Tumor
  • Folic Acid / chemistry*
  • Humans
  • Male
  • Mice
  • Mice, Nude
  • Nanoparticles / chemistry*
  • Prostatic Neoplasms / radiotherapy*
  • RNA, Small Interfering / therapeutic use*
  • Radiation Tolerance
  • Radiation-Sensitizing Agents / therapeutic use*
  • Xenograft Model Antitumor Assays

Substances

  • Androgen Receptor Antagonists
  • RNA, Small Interfering
  • Radiation-Sensitizing Agents
  • Folic Acid